毛蕊异黄酮-磷脂复合物的处方研究  

Formulation optimization of calycosin phospholipid complex

作　　者：史卓琪 刘黎瑶 熊倩 王庆奎[2] SHI Zhuo-qi;LIU Li-yao;XIONG Qian;WANG Qing-kui(Department of Biopharmaceuticals,College of Basic Science,Tianjin Agricultural University,Tianjin 300384,China;Tianjin Key Lab of Aquatic Ecology and Aquaculture,Tianjin Agricultural University,Tianjin 300384,China)

机构地区：[1]天津农学院基础科学学院生物制药系,天津300384 [2]天津农学院天津市水产生态及养殖重点实验室,天津300384

出　　处：《天津农学院学报》2019年第4期77-82,共6页Journal of Tianjin Agricultural University

基　　金：天津市教委科研计划项目(2017KJ181);天津市水产产业技术体系创新团队项目(ITTFRS2017004);国家自然科学基金面上项目(31170442)

摘　　要：毛蕊异黄酮是从黄芪中提取分离得到的小分子异黄酮类活性化合物,可与机体的雌激素受体结合发挥显著的雌激素样作用、抗肿瘤和免疫调节等作用。但由于其脂溶性差等问题,造成制剂成型性差,体内生物利用度低。本研究旨在利用磷脂复合技术提高其脂溶性。其中,通过溶剂-旋转蒸发法,以复合率(AE)为筛选指标,通过单因素筛选以及正交设计,筛选得到制备毛蕊异黄酮-磷脂复合物的最佳处方。优选复合条件下,毛蕊异黄酮与大豆磷脂的复合比例为1∶5;复合溶剂为pH 6.0的无水乙醇;复合时间为60 min,在该优选处方工艺下,毛蕊异黄酮-磷脂复合率达到90%以上,4℃下可稳定保存3个月。该研究为毛蕊异黄酮-磷脂复合物的后期应用奠定了物质基础。Calycosin is an active substance extracted and separated from Astragalus membranaceus.It could combine with estrogen receptor and generate estrogen-like action,antitumor and immunoregulation effect.However,because of its poor lipophilicity,it is difficult to be utilized in medical preparation.And its in vivo bioavailability is usually extremely low.This study was designed to increase the lipophilicity of calycosin using phospholipid complexation technology.In this study,associative efficiency(AE)was set as screening parameter and optimal formulation of calycosin phospholipid complex was obtained using solvent evaporation method based on single factor screening and orthogonal design.Under the selected formulation,mass ratio of calycosin to phospholipid was 1∶5 and composite time was 60 minutes in ethanol of pH 6.0.For the selected formulation,AE of calycosin phospholipid complex could reach 90% and storage stability remained in 3 months under 4℃.Compared with calycosin material medicine,the lipophilicity of phospholipid complex was increased by 600 times,which provides the basis for practical application.

关 键 词：毛蕊异黄酮 磷脂复合物 正交设计 处方筛选 

分 类 号：P641.131[天文地球—地质矿产勘探] S152.72[天文地球—地质学]